eALM1192
eALM1192 is a selective mTOR kinase inhibitor (IC50 = 2.3 nM) that also inhibits DNA-PK (IC50 = 84 nM), PI3Kα, and PKN3, with 37-fold selectivity for mTOR over DNA-PK. eALM1192 exhibits antiproliferative activity against cancer cell lines and colorectal cancer cell lines. eALM1192 can be used for colorectal cancer research.
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- CAS No.: 3134761-90-0
- Formule: C23H23N7O3
- Masse moléculaire:445.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
mTOR 2.3 nM (IC50) |
DNA-PK 84 nM (IC50) |
PI3Kα |
PKN3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW48 | EC50 |
5.6 nM
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Antiproliferative activity against human SW48 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
Antiproliferative activity against human SW48 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
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D6MD00572A |
| HCT-116 | EC50 |
49 nM
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Antiproliferative activity against human HCT116 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
Antiproliferative activity against human HCT116 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
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D6MD00572A |
| SW480 | EC50 |
63 nM
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Antiproliferative activity against human SW480 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
Antiproliferative activity against human SW480 colorectal cancer cells assessed as reduction in cell viability incubated for 5 days by PrestoBlue assay.
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D6MD00572A |
In Vitro
2w (eALM1192) (1-10000 nM; 5 days) exhibits potent low-nanomolar antiproliferative activity across SW48, HCT116 and SW480 colorectal cancer cell lines[1].
eALM1192 (1 μM) acts as a highly selective inhibitor, demonstrating potent activity (determined as residual activity at 1 μM) primarily against MTOR, DNAPK, and PIK3CA/PIK3R1.
2w (eALM1192) (0.09-3000 nM) is a potent mTOR inhibitor with an IC50 of 2.3 nM and 37-fold selectivity over DNA-PK[1].
2w (eALM1192) (1 µM; 0-45 min) demonstrates excellent metabolic stability with a half-life of 109 min in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 3134761-90-0
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Masse moléculaire 445.47
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Formule C23H23N7O3
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SMILES
O=C(N1CCC(CN2C=C(C3=CC=C(OC(N)=N4)C4=C3)C5=C(N)N=CN=C52)CC1)OCC#C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
eALM1192 Related Classifications
HY-189486 Related Classifications
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